CAS 878739-06-1|AZ 628

Introduction:Basic information about CAS 878739-06-1|AZ 628, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameAZ 628
CAS Number878739-06-1Molecular Weight451.520
Density1.2±0.1 g/cm3Boiling Point/
Molecular FormulaC27H25N5O2Melting Point/
MSDSUSAFlash Point/
Symbol
GHS06
Signal WordDanger

Names

Name3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide
SynonymMore Synonyms

AZ 628 BiologicalActivity

DescriptionAZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
Related CatalogSignaling Pathways >>MAPK/ERK Pathway >>RafResearch Areas >>Cancer
Target

c-Raf-1:29 nM (IC50)

B-RafV600E:34 nM (IC50)

B-Raf:105 nM (IC50)

In VitroAZ628 reduces activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC50 values of 105, 34 and 29 nM, respectively. AZ628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation[1]. AZ-628 suppresses growth in cells expressing K-RASG13D. Inhibition of RAF with AZ-628 suppresses MEK and ERK phosphorylation. AZ-628 selectively affects viability in K-RAS mutant cells[2].
Cell AssayCell viability quantified by Syto60 after 72 hours of AZ-628 (0.5, 1.0, and 1.5 μM), CI-1040 or BAY61-3606 treatment in HCT-116 (K-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines. Relative cell viability is normalized to DMSO vehicle treated control for each cell line[2].
References

[1]. Khazak V, et al. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609.

[2]. Lau KS, et al. BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012;7(7):e41343.

Chemical & Physical Properties

Density1.2±0.1 g/cm3
Molecular FormulaC27H25N5O2
Molecular Weight451.520
Exact Mass451.200836
PSA99.81000
LogP2.78
Appearance of Characterswhite to beige
Index of Refraction1.638
InChIKeyZGBGPEDJXCYQPH-UHFFFAOYSA-N
SMILESCc1ccc(NC(=O)c2cccc(C(C)(C)C#N)c2)cc1Nc1ccc2ncn(C)c(=O)c2c1
Storage condition?20°C
Water SolubilityDMSO: soluble10mg/mL, clear

Safety Information

Symbol
GHS06
Signal WordDanger
Hazard StatementsH301-H315-H319-H335
Precautionary StatementsP261-P301 + P310-P305 + P351 + P338
Hazard CodesT
Risk Phrases25-36/37/38
Safety Phrases26-36/37/39-45
RIDADRUN 2811 6.1 / PGIII
Hazard Class6.1
HS Code2933990090

Customs

HS Code2933990090
Summary2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

cc-82
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-
AZ628
3-(2-Cyano-2-propanyl)-N-{4-methyl-3-[(3-methyl-4-oxo-3,4-dihydro-6-quinazolinyl)amino]phenyl}benzamide
AZ 628
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